220389-06-0Relevant academic research and scientific papers
Synthesis and conformation of dipeptide taste ligands containing homo-β-amino acid residues
Isernia,Bucci,De Napoli,Di Lello,Iacovino,Montesarchio,Piccialli,Rossi,Saviano,Benedetti
, p. 577 - 587 (1999)
The synthesis and conformational properties of a series of dipeptide taste ligands, differing from the commercial sweetener aspartame by the presence of a methylene group between the Cα and the C′ carbon atoms (as in homo-β-residues) in either the L-Asp or the L-Phe residues, are described. Homo-β-residues such as homo-β-aspartic acid, homo-β-phenylglycine and homo-β-phenylalanine, obtained by homologation of the corresponding proteinogenic α-amino acids, have been used in the solution peptide synthesis of the following aspartame analogues in protected and unprotected forms: NH2-homo-β-(L or D)-Asp-L-Phe-OMe, NH2-L-Asp-homo-β-L-Phg-OMe and NH2-L-Asp-homo-β-L-Phe-OMe. Lengthening of the peptide skeleton at the L-Asp site results in a drastic loss of sweetness with the production of tasteless compounds; on the other hand, lengthening of the skeleton at the C-terminal L-Phe site partially mantains the sweet taste in both NH2-L-Asp-hamo-β-L-Phe-OMe and NH2-L-Asp-homo-β-L-Phg-OMe. The solution conformation of the synthesized dipeptide taste ligands was investigated by NMR and circular dichroism techniques. The analysis of NMR data combined with restrained molecular dynamics calculations shows that all peptides are fairly flexible and they do not assume a preferred conformation in DMSO and methanol. The peptides containing homo-β-L-Phe and homo-β-L-Phg do adopt a discrete number of conformation among which mainly extended and 'L-shaped' conformation are represented The circular dichroism spectra are consistent with the NMR results, indicating a significant flexibility for these compounds. Copyright
Lactone integrin antagonists
-
, (2008/06/13)
The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or the αvβ5 integrin.
Hydroxy acid integrin antagonists
-
, (2008/06/13)
The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or the αvβ5 integrin.
N-acylamino acid amide compounds and intermediates for preparation thereof
-
, (2008/06/13)
The present invention discloses the compound represented by the formula (I): wherein A represents the following formula (a-1) or the following formula (a-2): B represents the following formula (b): (wherein the symbols are each as defined in the specification) or a pharmaceutically acceptable salts thereof, and intermediates for the preparation thereof, which have excellent platelet aggregation inhibitory activity and other properties and useful as prophylactic or therapeutic agents for diseases associated with a fibrinogen receptor, thrombosis, infarction and the like.
Aminobenzamidinosuccinyl lactone derivatives useful as inhibitors of platelet aggregation
-
, (2008/06/13)
This invention provides a compound of the formula or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutical compositions of such compounds and a method of treatment to inhibit aggregation of platelets.
Platelet aggregation inhibitors
-
, (2008/06/13)
This invention relates to compounds having the following formula STR1 or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
